Assay Detail
Binding
CHEMBL4182859
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at GAL4-tagged human LXRalpha assessed as receptor activation expressed in African green monkey CV1 cells by luciferase reporter gene assay
27
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 6.24 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4209665 | — | — | 1 | 7.16 |
| CHEMBL4212458 | — | — | 1 | 6.79 |
| CHEMBL4210791 | — | — | 1 | 6.72 |
| CHEMBL4217890 | — | — | 1 | 6.60 |
| CHEMBL4212995 | — | — | 1 | 6.58 |
| CHEMBL4206412 | — | — | 1 | 6.54 |
| CHEMBL4208087 | — | — | 1 | 6.51 |
| CHEMBL4204747 | — | — | 1 | 6.50 |
| CHEMBL4206368 | — | — | 3 | 6.50 |
| CHEMBL4209091 | — | — | 1 | 6.47 |
| CHEMBL62136 | T091317 | — | 1 | 6.45 |
| CHEMBL4218626 | — | — | 1 | 6.43 |
| CHEMBL4217418 | — | — | 1 | 6.42 |
| CHEMBL4213493 | — | — | 1 | 6.01 |
| CHEMBL4205428 | — | — | 1 | 6.01 |
| CHEMBL4214055 | — | — | 1 | 5.99 |
| CHEMBL4209808 | — | — | 1 | 5.89 |
| CHEMBL4216643 | — | — | 1 | 5.68 |
| CHEMBL4214020 | — | — | 1 | 5.62 |
| CHEMBL4214711 | — | — | 1 | 5.56 |
| CHEMBL4214210 | — | — | 1 | 5.55 |
| CHEMBL4213534 | — | — | 1 | 5.48 |
| CHEMBL4218423 | — | — | 1 | - |
| CHEMBL4215334 | — | — | 1 | - |
| CHEMBL4212978 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4209665 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4212458 | — | EC50 | = | 163.0 | nM | 6.79 |
| CHEMBL4210791 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4217890 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4212995 | — | EC50 | = | 265.0 | nM | 6.58 |
| CHEMBL4206412 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4208087 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4204747 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4206368 | — | EC50 | = | 315.0 | nM | 6.50 |
| CHEMBL4209091 | — | EC50 | = | 342.0 | nM | 6.47 |
| CHEMBL62136 | T091317 | EC50 | = | 359.0 | nM | 6.45 |
| CHEMBL4218626 | — | EC50 | = | 374.0 | nM | 6.43 |
| CHEMBL4217418 | — | EC50 | = | 385.0 | nM | 6.42 |
| CHEMBL4206368 | — | EC50 | = | 792.0 | nM | 6.10 |
| CHEMBL4205428 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4213493 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4214055 | — | EC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL4209808 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4216643 | — | EC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL4214020 | — | EC50 | = | 2403.0 | nM | 5.62 |
| CHEMBL4214711 | — | EC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL4214210 | — | EC50 | = | 2820.0 | nM | 5.55 |
| CHEMBL4213534 | — | EC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL4206368 | — | EC50 | > | 7500.0 | nM | - |
| CHEMBL4215334 | — | EC50 | > | 7500.0 | nM | - |
| CHEMBL4218423 | — | EC50 | > | 7500.0 | nM | - |
| CHEMBL4212978 | — | EC50 | > | 7500.0 | nM | - |